75 results about "Fluorouracilum" patented technology

The invention discloses an enantiokaurane compound with antitumor activity as well as a preparation method and application of the enantiokaurane compound. According to the present invention, chemical components of Western African plant I.trichantha tubers are deeply studied, and a variety of chromatographic separation methods such as macroporous resin, silica gel resin, medium pressure preparation-MCI column, gel normal pressure column and semi-preparative high performance liquid chromatography are combined to separate to obtain one enantiokaurane new compound Trichanthone B; experiments show that the compound obtained through separation has a good inhibition effect on an MIA PaCa-2 pancreatic cancer cell line and an A549 lung cancer cell line, and IC50 of the compound on the MIA PaCa-2 pancreatic cancer cell line reaches a nanomole level; the effect of the compound is stronger than that of positive drugs 5-fluorouracil and carboplatin, and the compound has the potential of being developed into new drugs for resisting pancreatic cancer and lung cancer.

This invention relates to a pharmaceutical composition for tumor treatment and its application. Specifically, this invention relates to a composition containing a fluorouracil drug and pyrimidine nucleosides and their derivatives. Fluorouracil drugs and pyrimidine nucleotides and their derivatives have a synergistic antitumor effect; combined use can reduce the concentration of single drugs and achieve better antitumor efficacy, while reducing toxic side effects.

The application provides a combination drug of a PLA2G7 inhibitor and a chemotherapeutic drug and its use in resisting triple-negative breast cancer, and belongs to the technical field of medicines. The combination drug is a PLA2G7 inhibitor and a chemotherapeutic drug in the same or different specifications of unit preparations for simultaneous or separate administration, and a pharmaceutically acceptable carrier. The application first discovers and proves that the PLA2G7 inhibitor Darapladib can significantly enhance the anti-tumor activity of paclitaxel, 5-fluorouracil or cisplatin on triple-negative breast cancer, and meanwhile, the combination of the PLA2G7 inhibitor and paclitaxel has a synergistic effect in down-regulating the phosphorylation level of STAT3 protein in cancer cells and inhibiting the growth and proliferation of cancer cells; the combination of the PLA2G7 inhibitor and 5-fluorouracil also shows a synergistic effect in inhibiting the growth and proliferation of cancer cells. The application provides a new and effective combination drug strategy for improving the treatment effect of the chemotherapeutic drug on triple-negative breast cancer.

The application relates to a synthesis method of red luminescent carbon dots with a targeting diagnosis and treatment potential of hepatocellular carcinoma, which comprises the following steps: 1) adding 5-fluorouracil and indocyanine green into deionized water, uniformly mixing, and forming a uniform mixed solution; 2) heating the mixed solution obtained in the step 1) at 160-200 DEG C for 5-9 h, and cooling to room temperature; 3) filtering and dialyzing the solution obtained in the step 2), and obtaining a pure 5-FICD solution; and 4) freeze-drying the solution obtained in the step 3), and obtaining the product. The method takes anticancer drug 5-fluorouracil and photosensitizer indocyanine green as precursors, synthesizes a low-toxicity red light carbon dot through a simple hydrothermal method, improves the shortcoming that a chemotherapy drug has a large side effect, and realizes the targeted killing of hepatocellular carcinoma cells.

The application belongs to the technical field of medicine, and relates to a use of minocycline in preparation of an antitumor synergist. The minocycline, as the antitumor synergist, has a synergistic effect with 5-fluorouracil and gemcitabine, significantly enhances the curative effect of an antitumor drug, reduces the dosage of the antitumor drug, and reduces side effects of the antitumor drug on the body or damage of the antitumor drug to normal tissue cells.

The application belongs to the technical field of medicine preparation, and particularly relates to a magnetic layered double hydroxide, a targeted drug-loaded nano preparation, a preparation method and application of a tumor-targeted drug-loaded nano preparation. The preparation method of the magnetic layered double hydroxide provided by the application can prepare Fe3O4 nanoparticles with small particle size, and further prepare the magnetic layered double hydroxide which can be used as a water-soluble drug carrier. The magnetic layered double hydroxide is used for preparing the targeted drug-loaded nano preparation and the tumor-targeted drug-loaded nano preparation, and can be used for delivering water-soluble drugs such as 5-fluorouracil. The tumor-targeted drug-loaded nano preparation has good dispersity and can be actively targeted to HepG2 cells with high FR expression, has a good inhibitory effect on liver cancer cells, and is expected to provide a potential new treatment system for magnetic chemotherapy.

An implant device for an eye disease to be inserted into an eyeball may include: a tube having one end to be inserted into an anterior chamber of the eyeball, the tube including a hollow portion through which aqueous humor is drained; and a matrix coupled to an outer surface of the tube and formed of a material capable of impregnating and releasing a drug. At least a part of the matrix may have a cross-section larger than a diameter of the tube. When the implant device for an eye disease is used, an antifibrotic agent, such as dexamethasone, mitomycin-C (MMC), 5-fluorouracil (5-FU), triamcinolone (TA), an anti-vascular endothelial growth factor (VEGF) inhibitor, or a transforming growth factor-beta-beta (TGF-β) inhibitor may be loaded on the matrix, and the antifibrotic agent may be released to surrounding tissue from the matrix after the implant device is inserted.

The present invention belongs to the technical field of pharmaceutical chemistry, and discloses a paeonol Mannich base-rhein conjugate, a preparation method thereof and an application thereof. The conjugate is a compound represented by the general formula (I) or (II) or a pharmaceutically acceptable salt thereof. Compared with the clinically commonly used anti-tumor drugs fluorouracil and paeonol, the conjugate of the present invention has significantly higher in vitro proliferation inhibitory activities against human liver cancer cells (HepG2) and human lung cancer cells (A549), and the in vitro proliferation inhibitory activities of most compounds against human cervical cancer cells (Hela), human colon cancer cells (HT29) and human osteosarcoma cells (U2OS) are significantly better than those of fluorouracil and paeonol, indicating excellent anti-tumor effects. Moreover, the conjugate of the present invention has good water solubility and is expected to be applied to the treatment of various cancers such as cervical cancer, colon cancer, osteosarcoma, lung cancer or liver cancer, and has broad clinical application prospects.

This invention provides a sample pretreatment method and identification method for identifying ginseng polysaccharides in compound fluorouracil oral solution, belonging to the field of pharmaceutical detection and analysis technology. The sample pretreatment method of this invention includes: centrifuging the compound fluorouracil oral solution and taking the clear solution; adding silica gel to the clear solution, mixing, and removing the solvent to obtain a solid mixture; adding ethanol solution or anhydrous ethanol to the obtained solid mixture, heating and refluxing, discarding the ethanol solution, and obtaining the residue; adding water to the obtained residue, sequentially extracting and centrifuging, taking the supernatant obtained by centrifugation, removing the solvent from the supernatant, and then redissolving it with water; the identification method of this invention is thin-layer chromatography analysis, and the developing solvent includes the following components in parts by volume: 6.8-9.2 parts of n-propanol, 1.76-2.24 parts of water, 0.75-1.24 parts of ethyl acetate, and 0.75-1.24 parts of glacial acetic acid. The sample pretreatment method and identification method for identifying ginseng polysaccharides in compound fluorouracil oral solution of this invention have high specificity.

The application belongs to the technical field of biological medical materials, and provides a preparation method of an E. coli drug preparation with photosensitive drug release, which comprises the following steps: incubating photosensitizer Ce6 nanoparticles and E. coli carrying 5-fluorouracil and extract of Prunella vulgaris to obtain the drug preparation; wherein the E. coli carrying 5-fluorouracil and extract of Prunella vulgaris is obtained by using a high-voltage electroporation method to transfer 5-fluorouracil and extract of Prunella vulgaris into the E. coli; the photosensitizer Ce6 nanoparticles are prepared by adding tripolyphosphate to a Ce6 chitosan solution; and the extract of Prunella vulgaris is obtained by extracting Prunella vulgaris with water, concentrating and drying the extract. The traditional antitumor drug 5-fluorouracil and the extract of Prunella vulgaris are matched with each other, and a synergistic effect in the aspect of antitumor is generated, thereby providing a certain reference value for development of a new antitumor drug combination and preparation.

The present invention belongs to the field of medicine and specifically relates to the use of a combination of astemizole and terfenadine in the preparation of a drug for treating gastric cancer. The present invention finds that the antihistamine drug terfenadine can enhance the inhibitory effect of astemizole on gastric cancer AGS and HGC27 cells, significantly inhibiting the proliferation of AGS and HGC27 gastric cancer cells. Furthermore, terfenadine and astemizole can inhibit the migration of gastric cancer cells, induce apoptosis of gastric cancer cells, and block the cell cycle. The effect of terfenadine and astemizole in inhibiting the proliferation of gastric cancer cells is superior to that of the commonly used clinical anticancer drug 5-fluorouracil (5-FU), and the present invention has good application prospects in the treatment of gastric cancer.

The invention discloses a NO / 5-fluorouracil double-delivery system based on Zn-MOF and application of the NO / 5-fluorouracil double-delivery system. A preparation method of the NO / 5-fluorouracil double-delivery system comprises the steps that IRMOF-3 serves as a carrier, 5-fluorouracil is loaded through physical adsorption, NO is loaded in a covalent binding mode under high pressure, and the pH-responsive double-drug delivery system IRMOF-3-NONO-5-FU is constructed. Experiments show that IRMOF-3-NONO (at) 5-FU has pH response release ability, efficient release of 5-FU and NO can be realized in a simulated tumor microenvironment (pH 5), and release of the IRMOF-3-NONO (at) 5-FU is significantly inhibited in a normal physiological environment (pH 7.4); a tumor cell toxicity test shows that the 5-fluorouracil and NO in the IRMOF-3-NONO-5-FU have a synergistic anti-tumor curative effect, and potential clinical application prospects are achieved.

A pharmaceutical composition for tumor vascular occlusion according to an exemplary embodiment may include alkaline 5-fluorouracil and glucose. For example, the composition may include glucose which exerts a synergistic effect on inducing apoptosis of vascular endothelial cells with alkaline 5-fluorouracil, thereby significantly enhancing the anti-cancer effect.

The invention specifically discloses a PreTA inhibitor and application thereof, and relates to the technical field of biological medicines. The inhibitor provided by the invention can be used for effectively inhibiting the activity of PreTA, so that the anti-tumor effect of 5-fluorouracil (5-FU) is recovered.

The application discloses a method for catalytically producing 5-fluorouracil and application, and belongs to the technical field of biology. The method uses 5-fluoroorotic acid as a substrate and orotidine-5'-phosphate decarboxylase as a catalyst to efficiently catalyze the synthesis of 5-fluorouracil. The catalytic efficiency is further improved by molecular modification of orotidine-5'-phosphate decarboxylase, the efficient and green production of 5-fluorouracil is realized, and the application of 5-fluorouracil in the fields of medicine and the like is promoted.

The application relates to a pharmaceutical cocrystal of cytarabine and 5-fluorouracil and a preparation method thereof, and relates to the technical field of pharmaceutical cocrystals. The pharmaceutical cocrystal is composed of one cytarabine molecule and one 5-fluorouracil molecule as a basic structural unit, and has a chemical formula of [C9H 13 N3O5.C4H3N2O2F]; the pharmaceutical cocrystal belongs to an orthorhombic system and has a space group of P212121. The pharmaceutical cocrystal prepared by a solvent evaporation method and a cooling method improves the permeability of cytarabine, appropriately reduces the solubility of cytarabine, and significantly improves the antitumor activity of cytarabine; through the complementary advantages of the properties and the pharmacodynamic effects of two components, the synergistic antitumor effects of cytarabine and 5-fluorouracil are realized, and a new idea is provided for developing synergistic antitumor pharmaceutical cocrystals. The pharmaceutical cocrystal can keep the skeleton structure of the crystal unchanged after long-term placement at room temperature, the preparation method is simple and easy to implement, the cost is low, and the pharmaceutical cocrystal is convenient for large-scale production.

The invention discloses synthesis and antitumor activity research of a novel drug small molecular formula (1) containing an indole structure, wherein R is as follows: 5-acetylvaleric acid is used as a starting raw material, then Fischer reaction, methylation reaction and hydrolysis reaction are performed to obtain 4-(5-(tert-butyl)-1, 2-dimethyl-1H-indole-3-yl) butyric acid, and the 4-(5-(tert-butyl)-1, 2-dimethyl-1H-indole-3-yl) butyric acid is used as a raw material. The compound is coupled with different amine compounds to obtain a target compound. A target compound is subjected to a CCK-8 experiment, and a conclusion is obtained that the target compound 6f and 5-fluorouracil are tested at the concentration of 20 [mu] M within 6a-6 h, and it can be known that the compound 6f has the best inhibition effect on A549 cells, Hela cells and A549 cells. IC50 value calculation is carried out on a target compound under various concentrations, the IC50 value of 6c to Hep G2 cells is minimum and the inhibition effect is best, and the IC50 value of 6f to A549 cells and Hela cells is minimum and the inhibition effect is best.

Disclosed are method of treating a subject in need thereof comprising applying an alternating electric field, at a frequency for a period of time, to a target site of the subject in need thereof; and administering a combination of leucovorin calcium, fluorouracil, irinotecane hydrochloride, and oxaliplatin to the subject in need thereof. Disclosed are methods of reducing viability of cancer cells comprising applying an alternating electric field, at a frequency for a period of time, to a population of cancer cells; and contacting the population of cells with a combination of leucovorin calcium, fluorouracil, irinotecane hydrochloride, and oxaliplatin. Disclosed are methods of increasing apoptosis of cancer cells comprising applying an alternating electric field, at a frequency for a period of time, to a population of cancer cells; and contacting the population of cancer cells with a combination of leucovorin calcium, fluorouracil, irinotecane hydrochloride, and oxaliplatin. Disclosed are methods of reducing the number of cancer cells comprising applying an alternating electric field, at a frequency for a period of time, to a population of cancer cells; and contacting the population of cancer cells with a combination of leucovorin calcium, fluorouracil, irinotecane hydrochloride, and oxaliplatin.

This invention discloses a method for scalable preparation of 5-fluorouracil-loaded lyophilized nanoparticles. The method first involves self-assembling 5-fluorouracil into a polymer carrier to form core-shell nanoparticles. Then, the hydrophobic core-shell nanoparticles undergo a double emulsification-isothermal evaporation process to form hydrophilic micro / nanoparticles. Finally, D-mannose is assembled onto the surface of the micro / nanoparticles, followed by gradient freeze-drying to prepare PLGA / 5-FU-loaded lyophilized nanoparticles. This method offers advantages such as simple operation, scalability, and good reproducibility. The 5-FU drug in the prepared lyophilized nanoparticles exhibits good crystallinity. During the inhibition of pancreatic cancer cell growth, it effectively improves the bioavailability, biocompatibility, and physical stability of 5-fluorouracil, significantly inhibiting pancreatic cancer cell growth and demonstrating high anti-tumor immunomodulatory properties.

The invention relates to an oligonucleotide lung targeting delivery system and application thereof in treatment of lung diseases, and relates to the technical field of biological medicines and nano-medicines. The invention designs a high-efficiency lung targeting oligonucleotide delivery drug, which comprises lipid nanoparticles, the lipid nanoparticles contain oligonucleotide and lipid components, and the lipid components are composed of 4-(N, N-dimethylamino) butyric acid (dilinoleyl) methyl ester, (2, 4-dimethylamino) butyric acid (dilinoleyl) methyl ester, (2, 4-dimethylamino) butyric acid (2, 4-dimethylamino) butyric acid (2, 4-dimethylamino) butyric acid (2, 4-dimethylamino) butyric acid (2, 4-dimethylamino) butyric acid The composition is composed of 1, 3-dioleoyl-propyl)-trimethylamine, dipalmitoyl phosphatidylcholine and pegylated lipid. A breakthrough of a nucleic acid medicine lung delivery technology is realized, in-vivo experiment verification results show that the lung aggregation efficiency is improved by about 2-4 times compared with that of traditional lipid nanoparticles, the lipid nanoparticles have remarkable lung metastatic tumor resisting activity, in-vivo experiments show that the lipid nanoparticles can inhibit growth of colorectal cancer lung metastatic tumors and prolong the survival time of mice, and the lipid nanoparticles have good application prospects. And the effect is better than that of 5-fluorouracil and regorafenib.

The invention belongs to the technical field of biological medicine, and particularly discloses fluorouracil sustained-release nano-microspheres as well as a preparation method and application thereof. The preparation method comprises the following steps: S1, dissolving fluorouracil in a polyarginine aqueous solution, uniformly stirring, and adjusting the pH value to 7.2-7.4 to obtain a fluorouracil solution; s2, dissolving amphiphilic alginate in water, sequentially adding carboxymethyl chitosan and quaternized gelatin, and uniformly stirring to obtain a composite carrier solution; and S3, mixing the fluorouracil solution obtained in the step S1 with the composite carrier solution obtained in the step S2, performing ultrasonic treatment, performing self-assembly, performing centrifugation, and collecting precipitates to obtain the fluorouracil nano-microspheres. The invention discloses a fluorouracil sustained-release nano-microsphere as well as a preparation method and application thereof. The fluorouracil sustained-release nano-microsphere can be used for remarkably improving the encapsulation efficiency and the drug loading capacity of fluorouracil, realizing long-acting sustained release of drugs, enhancing the tumor targeting property and the cell uptake efficiency and improving the treatment effect.

The present invention belongs to the field of biomedical technology, and particularly relates to a pyridinecarboxylic acid alkaloid, its preparation method and application. This compound can be obtained by using a fungus derived from sea lilies in the South China Sea through modern microbial fermentation engineering technology, and it is easy to achieve large-scale industrial production. Moreover, it is found through research that the pyridinecarboxylic acid alkaloid compound has a significant inhibitory effect on gastric cancer cells, can significantly inhibit the activity and clone formation of gastric cancer cells, promote the apoptosis of gastric cancer cells, and reduce the invasion of gastric cancer cells; when the pyridinecarboxylic acid alkaloid compound and a first-line clinical chemotherapy drug such as 5-fluorouracil act on gastric cancer cells in combination, the cell inhibition effect is also significantly improved, showing a synergistic anti-gastric cancer effect.

The present invention discloses the use of a lncRNA IGFL2-AS1 gene inhibitor in the preparation of a drug for treating lung cancer. The nucleotide sequence of the lncRNA IGFL2-AS1 gene is shown in SEQ ID NO.1. The lncRNA IGFL2-AS1 gene inhibitor is a small interfering RNA that uses the IGFL2-AS1 gene or its transcript as an inhibition target or a silencing target. The nucleotide sequence of the shRNA of the small interfering RNA is shown in SEQ ID NO.17 or SEQ ID NO.18. IGFL2-AS1 is mainly localized in the cell nucleus and expressed in a small amount in the cytoplasm. IGFL2-AS1 can promote the proliferation, migration and drug resistance of non-small cell lung cancer A549 and H520 cells. Targeted inhibition of IGFL2-AS1 can significantly reduce the drug resistance of lung cancer cells to cisplatin or 5-fluorouracil.

The invention discloses a 5-fluorouracil atropine double-drug sustained release preparation based on temperature-sensitive hydrogel as well as a preparation method and application of the 5-fluorouracil atropine double-drug sustained release preparation. The double-drug sustained release preparation is prepared from the following raw materials: a vagus nerve blocking agent, 5-fluorouracil (5-FU) and temperature-sensitive hydrogel (PLEL), wherein the vagus nerve blocking agent comprises atropine. According to the invention, the chemotherapeutic drug 5-FU and the vagus nerve signal blocking agent (such as atropine) are co-delivered through the temperature-sensitive hydrogel for the first time to realize'double strike 'on gastric cancer tumors, that is, tumor cells are directly killed and cancer-promoting nerve signals are blocked, so that the treatment effect on gastric cancer is remarkably improved. Besides, the double-drug sustained-release preparation is high in safety and good in sustained-release effect, 5-FU and the vagus nerve blocker can be accurately delivered to a tumor area through local injection and in-situ gelation of the temperature-sensitive hydrogel, whole-body exposure of the drug is reduced, local residence time is prolonged, and toxic and side effects are reduced.

The preparation tank comprises a tank body and four supporting legs fixed to the lower end of the tank body, the upper end and the lower end of the tank body are each provided with an opening, the two ends of the upper end of the tank body are each rotationally connected with a cover plate corresponding to the opening, and bolts are inserted into the sides, away from the tank body, of the cover plates. The cover plate is fixed to the tank body through bolts, a storage groove is formed in the position, close to the top, in the tank body, a fourth pipeline communicated with an external high-pressure water source is fixedly inserted into the top in the storage groove, the upper end of the fourth pipeline penetrates through the tank body, and a fixing plate arranged in a 7 shape is fixedly connected to the upper end of the tank body; a servo motor is fixedly connected to the lower side wall of the fixing plate, and a vertically-arranged first pipeline is arranged in the tank body. According to the utility model, the plurality of pipelines are arranged, so that a user can conveniently wash the inner wall while the stirring operation of materials is not influenced, and the convenience and the practicability are improved.

The invention discloses an integrated electrochemical membrane reactor based on in-situ deep purification of high-salinity wastewater and a water treatment method of the integrated electrochemical membrane reactor. A ceramic membrane is used as a substrate, an iron-based non-metal coordination porous carbon active layer modified on the surface is used as a cathode, and the integrated electrochemical membrane reactor with catalytic oxidation and filtering functions is jointly formed by the ceramic membrane and an anode. The method is suitable for treating high-salt and degradation-resistant organic wastewater, can efficiently remove more than 90% of typical pollutants such as 5-fluorouracil and stably remove more than 50% of wastewater COD (Chemical Oxygen Demand) in a continuous flow operation mode, has the advantages of high catalytic activity, stable structure, flexible operation mode and the like, and is suitable for industrial production. And an efficient and reliable technical solution is provided for deep purification of the high-salt degradation-resistant wastewater.

The invention discloses a drug-loaded microgel-gel sustained-release dressing as well as a preparation method and application of the drug-loaded microgel-gel sustained-release dressing. The dressing comprises a drug microgel phase loaded by GelMA microspheres and a hydrogel shell phase formed by copolymerizing CSMA and a double-bond-containing micromolecule cross-linking agent, and can be polymerized and cured in situ through ultraviolet light. The carried medicine comprises one of bevacizumab, triamcinolone acetonide and fluorouracil, and multi-medicine synergistic slow release is achieved. The dressing provided by the invention has good biocompatibility, degradability, shape adaptability and slow release performance, can significantly improve local drug concentration, reduce administration frequency and improve patient compliance, and is suitable for treatment and repair of keloid.

The invention discloses a corynebacterium glutamicum target gene random mutation tool based on adenine deaminase and RNA polymerase and application of the corynebacterium glutamicum target gene random mutation tool, and belongs to the technical field of bioengineering. The uracil phosphoribosyltransferase encoding gene upp is successfully subjected to random mutation by using the method provided by the invention, a 5-fluorine-uracil resistant strain is obtained, the upp gene in the resistant strain is sequenced, and a mutation point causing the generation of 5-fluorine-uracil resistance is identified. According to the target gene random mutation method disclosed by the invention, the blank that corynebacterium glutamicum lacks large-fragment target gene random mutation is filled, and a powerful tool is provided for in-vivo directional mutation of large-fragment genes.

The invention discloses a compound RMY-186, a preparation method of the compound RMY-186 and application of the compound RMY-186 in drugs for treating drug-resistant tumors. The drugs further comprise chemotherapeutic drugs (including fluorouracil and oxaliplatin) which are used in a combined mode. The compound RMY-186 provided by the invention can directly promote the degradation of CAD regardless of whether mutation occurs or not. The chemotherapy effects of fluorouracil and the like are enhanced by promoting GC and CRC cell death and GSDME splitting decomposition. In conclusion, the RMY-186 can be used as a drug and a lead compound for overcoming GC and CRC chemotherapy drug-resistant tumors caused by CAD cleavage site mutation.

The invention provides a 5-HMF aptamer, an optimization method and application, the 5-HMF aptamer is one of the following sequences: H1-21m: SEQ ID NO1 sequence, H1-21m-5Fu-d: replacing T at the 20th site in the SEQ ID NO1 sequence with 5Fu, or H1-21mdUb: replacing T at the 13th site in the SEQ ID NO1 sequence with U, and the 5-HMF aptamer is one of the following sequences: H1-21m: SEQ ID NO1 sequence, H1-21m-5Fu-d: replacing T at the 20th site in the SEQ ID NO1 sequence with 5Fu, or H1-21mdUb: replacing T at the 13th site in the SEQ ID NO1 sequence with U. According to the 5-HMF aptamer provided by the invention, thymine at a key site of a truncated body is systematically replaced with uracil and 5-fluorouracil which are similar in structure, so that the binding affinity of the aptamer and the 5-HMF is remarkably enhanced, and a 5-HMF detection method based on a non-labeled aptamer is constructed.